Document Detail


A potent antagonist of the strychnine insensitive glycine receptor has anticonvulsant properties.
MedLine Citation:
PMID:  2560979     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
5.7-Dinitro-quinoxaline-2.3-dione (MNQX) displaced [3H]glycine binding to cortical membranes but had no effect n [3H]3-((+/-)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid ([3H]CPP) binding. MNQX potently antagonized N-methyl-D-aspartate (NMDA)-evoked release of [3H]GABA from cultured cortical neurones, NMDA evoked spreading depression and NMDA depolarizations in the rat neo-cortex. All of these responses were reversed by addition of glycine to the perfusion media. These results suggested that MNQX is an antagonist at the strychnine-insensitive glycine receptor associated with the NMDA receptor/ionophore complex. Furthermore the compound was found to antagonise audiogenic seizures in DBA-2 mice indicating the potential of glycine antagonists of this type in anticonvulsant therapy.
Authors:
M J Sheardown; J Drejer; L H Jensen; C E Stidsen; T Honoré
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  174     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1989 Dec 
Date Detail:
Created Date:  1990-05-02     Completed Date:  1990-05-02     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  197-204     Citation Subset:  IM    
Affiliation:
A/S Ferrosan, CNS Division, Sydmarken, Soeborg, Denmark.
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MeSH Terms
Descriptor/Qualifier:
Animals
Anticonvulsants*
Aspartic Acid / analogs & derivatives,  pharmacology
Cerebral Cortex / drug effects,  metabolism
Cortical Spreading Depression / drug effects
Female
Glycine / metabolism,  pharmacology
Male
Mice
Mice, Inbred DBA
N-Methylaspartate
Pregnancy
Pyrrolidinones / pharmacology
Quinoxalines / pharmacology*
Rats
Receptors, Glycine
Receptors, Neurotransmitter / drug effects,  metabolism,  physiology*
Seizures / chemically induced,  physiopathology
Strychnine / pharmacology*
gamma-Aminobutyric Acid / metabolism
Chemical
Reg. No./Substance:
0/Anticonvulsants; 0/Pyrrolidinones; 0/Quinoxalines; 0/Receptors, Glycine; 0/Receptors, Neurotransmitter; 1003-51-6/HA 966; 125910-83-0/5,7-dinitroquinoxaline-2,3-dione; 56-12-2/gamma-Aminobutyric Acid; 56-40-6/Glycine; 56-84-8/Aspartic Acid; 57-24-9/Strychnine; 6384-92-5/N-Methylaspartate

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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